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Assay Detail

CHEMBL5337707

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Antagonist activity at ER-alpha (unknown origin) by ER-alpha coactivator assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Estrogen receptor (CHEMBL206)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis, biological evaluation, and stability studies of raloxifene mono- and bis-sulfamates as dual-targeting agents.
Zaraei SO, Dohle W, Anbar HS, El-Gamal R, Leblond B, Foster PA, Al-Tel TH, Potter BVL, El-Gamal MI.
Bioorg Med Chem (2024) 101 : 117645 -117645
PubMed 38401456 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 8.16 8.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL489 AFIMOXIFENE 3.0 1 8.42
CHEMBL1358 FULVESTRANT 4.0 1 7.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL489 AFIMOXIFENE IC50 = 3.8 nM 8.42
CHEMBL1358 FULVESTRANT IC50 = 13.0 nM 7.89